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A Comprehensive Review on the Role of Polymers in Ocular Drug Delivery

Paramjot, Wadhwa S, Sharma A, Singh SK, Vishwas S, Kumar R, et al.

Curr Drug Deliv, 2024;21(1):16-37.
PMID: 36627785 DOI: 10.2174/1567201820666230110140312

Amongst different routes of drug delivery systems, ophthalmic drug delivery still requires a careful investigation and strict parameter measurements because the eyes are one of the most sensitive parts of the body and require special attention. The conventional systems for eyes lead to rapid elimination of formulation and hence very small contact time on the ocular epithelium. The current review article covers various types of polymers used in ocular drug delivery along with their applications/ limitations. Polymers are widely used by researchers in prodrug techniques and as a penetration enhancer in ocular delivery. This article covers the role and use of different polymeric systems which makes the final formulation a promising candidate for ophthalmic drug delivery. The researchers are still facing multiple challenges in order to maintain the therapeutic concentration of the drug in the eyes because of its complex structure. There are several barriers that further restrict the intraocular entry of the drug. In order to remove/reduce such challenges, these days various types of polymers are used for ocular delivery in order to develop different drug carrier systems for better efficacy and stability. The polymers used are highly helpful in increasing residence time by increasing the viscosity at the ocular epithelium layer. Such preparations also get easily permeated in ocular cells. The combination of different polymeric properties makes the final formulation stable with prolonged retention, high viscosity, high permeability, and better bioavailability, making the final formulation a promising candidate for ocular drug delivery.

Matched MeSH terms: Drug Carriers/chemistry
Fulltext Cytotoxicity Enhancement of α-Mangostin with Folate-Conjugated Chitosan Nanoparticles in MCF-7 Breast Cancer Cells

Herdiana Y, Wathoni N, Shamsuddin S, Muchtaridi M

Molecules, 2023 Nov 14;28(22).
PMID: 38005306 DOI: 10.3390/molecules28227585

α-mangostin (AM) is a promising natural anticancer agent that can be used in cancer research. However, its effectiveness can be limited by poor solubility and bioavailability. To address this issue, chitosan-based nanoparticles (CSNPs) have been investigated as a potential delivery system to enhance the cytotoxicity to cancer cells and improve selectivity against normal cells. In this study, we developed folate-conjugated chitosan nanoparticles (F-CS-NPs) using a carbodiimide-based conjugation method to attach folate to chitosan (CS), which have different molecular weights. The NPs were crosslinked using tripolyphosphate (TPP) via ionic gelation. To characterize the F-CS-NPs, we utilized various analytical techniques, including transmission electron microscopy (TEM) to evaluate the particle size and morphology, Fourier-transform infrared spectroscopy (FTIR) to confirm the presence of functional groups, and ultraviolet-visible spectroscopy (UV-Vis) to measure the absorption spectrum and confirm the presence of folate. The particle size of AM-F-CS-NPs ranged from 180 nm to 250 nm, with many having favorable charges ranging from +40.33 ± 3.4 to 10.69 ± 1.3 mV. All NPs exhibited the same spherical morphology. The use of F-CS-NPs increased drug release, followed by a sustained release pattern. We evaluated the cytotoxicity of AM, AM-F-CS-HMW, and AM-F-CS-LMW NPs against MCF-7 cells and found IC50 values of 8.47 ± 0.49, 5.3 ± 0.01, and 4.70 ± 0.11 µg/mL, respectively. These results confirm the improved cytotoxicity of AM in MCF-7 cells when delivered via F-CS-NPs. Overall, our in vitro study demonstrated that the properties of F-CS-NPs greatly influence the cytotoxicity of AM in MCF-7 breast cancer cells (significantly different (p < 0.05)). The use of F-CS-NPs as a drug-delivery system for AM may have the potential to develop novel therapies for breast cancer.

Matched MeSH terms: Drug Carriers/chemistry
Prevention of Hypercholesterolemia with "Liposomes in Microspheres" Composite Carriers: A Promising Approach for Intestinal-Targeted Oral Delivery of Astaxanthin

Liu A, He M, Liu C, Ye Z, Tan CP, Liu Y, et al.

J Agric Food Chem, 2024 Mar 27;72(12):6118-6132.
PMID: 38477232 DOI: 10.1021/acs.jafc.3c08697

Cardiovascular diseases are caused by hypercholesterolemia. Astaxanthin (AST) has been reported to exhibit antioxidant and anti-inflammatory properties. However, its bioavailability is poor because of low solubility and instability. In order to improve the bioavailability of AST, we developed an intestinal-responsive composite carrier termed as "liposomes in micropheres" incorporating N-succinyl-chitosan (NSC)-poly(ethylene glycol) (PEG) liposomes that functionalized by neonatal Fc receptors (FcRn) into hydrogels of sodium alginate (SA) and carboxymethyl chitosan (CMCS). In the AST NSC/HSA-PEG liposomes@SA/CMCS microspheres, the AST's encapsulation efficiency (EE) was 96.26% (w/w) and its loading capacity (LC) was 6.47% (w/w). AST NSC/HSA-PEG liposomes had stability in the gastric conditions and achieved long-term release of AST in intestinal conditions. Then, AST NSC/HSA-PEG liposomes@SA/CMCS bind to intestinal epithelial cell targets by the neonatal Fc receptor. In vitro permeation studies show that there was a 4-fold increase of AST NSC/HSA-PEG liposomes@SA/CMCS in AST permeation across the intestinal epithelium. Subsequent in vivo experiments demonstrated that the composite carrier exhibited a remarkable mucoadhesive capacity, allowing for extended intestinal retention of up to 12 h, and it displayed deep penetration through the mucus layer, efficiently entering the intestinal villi epithelial cells, and enhancing the absorption of AST and its bioavailability in vivo. And oral administration of AST NSC/HSA-PEG liposomes@SA/CMCS could effectively prevent hypercholesterolemia caused by a high-fat, high-cholesterol diet (HFHCD). These advancements highlight the potential of NSC/HSA-PEG liposomes@SA/CMCS composite carriers for targeted and oral uptake of hydrophobic bioactives.

Matched MeSH terms: Drug Carriers/chemistry
Effect of Different Carriers on In Vitro and In Vivo Drug Release Behavior of Aceclofenac Proniosomes

Sammour RMF, Chatterjee B, Taher M, Saleh MSM, Shahiwala A

Curr Drug Deliv, 2021;18(9):1272-1279.
PMID: 33605859 DOI: 10.2174/1567201818666210219105509

BACKGROUND: Improved bioavailability of Aceclofenac (ACE) may be achieved through proniosomes, which are considered as one of the most effective drug delivery systems and are expected to represent a valuable approach for the development of better oral dosage form as compared to the existing product. However, the carrier in this system plays a vital role in controlling the drug release and modulating drug dissolution. Accordingly, a comparative study on different carriers can give a clear idea about the selection of carriers to prepare ACE proniosomes.
OBJECTIVE: This study aims to evaluate the role of maltodextrin, glucose, and mannitol as carriers for in vitro and in vivo performance of Aceclofenac (ACE) proniosomes.
METHODS: Three formulations of proniosomes were prepared by the slurry method using the 100 mg ACE, 500 mg span 60, 250 mg cholesterol with 1300mg of different carriers, i.e., glucose (FN1), maltodextrin (FN2), and mannitol (FN3). In vitro drug release studies were conducted by the USP paddle method, while in vivo studies were performed in albino rats. Pure ACE was used as a reference in all the tests. Lastly, the results were analyzed using the High-Pressure Liquid Chromatography (HPLC) method, and data were evaluated using further kinetic and statistical tools.
RESULTS: No significant differences (p > 0.05) in entrapment efficiency (%EE) of FN1, FN2, and FN3 (82 ± 0.5%, 84 ± 0.66%, and 84 ± 0.34% respectively) were observed and formulations were used for further in vitro and in vivo evaluations. During in vitro drug release studies, the dissolved drug was found to be 42% for the pure drug, while 70%, 17%, and 30% for FN1, FN2, and FN3, respectively, at 15 min. After 24 hrs, the pure drug showed a maximum of 50% release while 94%, 80%, and 79% drug release were observed after 24 hr for FN1, FN2, and FN3, respectively. The in vivo study conducted on albino rats showed a higher Cmax and AUC of FN1 and FN2 in comparison with the pure ACE. Moreover, the relative oral bioavailability of proniosomes with maltodextrin and glucose as carriers compared to the pure drug was 183% and 112%, respectively. Mannitol- based formulation exhibited low bioavailability (53.7%) that may be attributed to its osmotic behavior.
CONCLUSION: These findings confirm that a carrier plays a significant role in determining in vitro and in vivo performance of proniosomes and careful selection of carrier is an important aspect of proniosomes optimization.

Matched MeSH terms: Drug Carriers
Functionalized chitosan for cancer nano drug delivery

Zaiki Y, Iskandar A, Wong TW

Biotechnol Adv, 2023 Oct;67:108200.
PMID: 37331671 DOI: 10.1016/j.biotechadv.2023.108200

Chitosan is a biotechnological derivative of chitin receiving a widespread pharmaceutical and biomedical applications. It can be used to encapsulate and deliver cancer therapeutics with inherent pH-dependent solubility to confer drug targeting at tumour microenvironment and anti-cancer activity synergizing cancer cytotoxic drug actions. To further reduce the off-target and by-stander adverse effects of drugs, a high targeted drug delivery efficiency at the lowest possible drug doses is clinically required. The chitosan has been functionalized with covalent conjugates or complexes and processed into nanoparticles to encapsulate and control drug release, to avoid premature drug clearance, to deliver drugs passively and actively to cancer site at tissue, cell or subcellular levels, and to promote cancer cell uptake of nanoparticles through membrane permeabilization at higher specificity and scale. Nanomedicine developed using functionalized chitosan translates to significant preclinical improvements. Future challenges related to nanotoxicity, manufacturability, selection precision of conjugates and complexes as a function of cancer omics and their biological responses from administration site to cancer target need critical assessments.

Matched MeSH terms: Drug Carriers
A review of recent advances of cellulose-based intelligent-responsive hydrogels as vehicles for controllable drug delivery system

Gong J, Hou L, Ching YC, Ching KY, Hai ND, Chuah CH

Int J Biol Macromol, 2024 Apr;264(Pt 2):130525.
PMID: 38431004 DOI: 10.1016/j.ijbiomac.2024.130525

To realize the maximum therapeutic activity of medicine and protect the body from the adverse effects of active ingredients, drug delivery systems (DDS) featured with targeted transportation sites and controllable release have captured extensive attention over the past decades. Hydrogels with unique three-dimensional (3D) porous structures present tunable capacity, controllable degradation, various stimuli sensitivity, therapeutic agents encapsulation, and loaded drugs protection properties, which endow hydrogels with bred-in-the-bone advantages as vehicles for drug delivery. In recent years, with the impressive consciousness of the "back-to-nature" concept, biomass materials are becoming the 'rising star' as the hydrogels building blocks for controlled drug release carriers due to their biodegradability, biocompatibility, and non-toxicity properties. In particular, cellulose and its derivatives are promising candidates for fabricating hydrogels as their rich sources and high availability, and various smart cellulose-based hydrogels as targeted carriers under exogenous such as light, electric field, and magnetic field or endogenous such as pH, temperature, ionic strength, and redox gradients. In this review, we summarized the main synthetic strategies of smart cellulose-based hydrogels including physical and chemical cross-linking, and illustrated the detailed intelligent-responsive mechanism of hydrogels in DDS under external stimulus. Additionally, the ongoing development and challenges of cellulose-based hydrogels in the biomedical field are also presented.

Matched MeSH terms: Drug Carriers
Nanomaterial Based Approaches for the Diagnosis and Therapy of Cardiovascular Diseases

Sharma PA, Maheshwari R, Tekade M, Tekade RK

Curr Pharm Des, 2015;21(30):4465-78.
PMID: 26354926

The increasing prevalence and complexity of cardiovascular diseases demand innovative strategies for diagnostic and therapeutic applications to improve patient care/prognoses. Additionally, various factors constrain present cardiovascular therapies, including low aqueous drug solubility, early metabolism, short half-life and drug delivery limitations. The efficient treatment of cardiovascular diseases requires improvement of traditional drug delivery systems. This can be accomplished by using novel nanomaterial that can incorporate diverse bio-actives along with diagnostic agents in a single carrier, referred to as theranostics. This review discusses the state of the art in the applications to diagnosis and therapy of innovative, nanomaterial- based strategies such as lipid based carriers, nanocapsules, magnetic nanoparticles, gold nanoparticles, protein conjugated nanoparticles, dendrimers and carbon-based nanoformulations with a special emphasis on how they can contribute to improving the management of cardiovascular disease.

Matched MeSH terms: Drug Carriers/chemistry
Cell-targeting aptamers act as intracellular delivery vehicles

Gopinath SC, Lakshmipriya T, Chen Y, Arshad MK, Kerishnan JP, Ruslinda AR, et al.

Appl Microbiol Biotechnol, 2016 Aug;100(16):6955-69.
PMID: 27350620 DOI: 10.1007/s00253-016-7686-2

Aptamers are single-stranded nucleic acids or peptides identified from a randomized combinatorial library through specific interaction with the target of interest. Targets can be of any size, from small molecules to whole cells, attesting to the versatility of aptamers for binding a wide range of targets. Aptamers show drug properties that are analogous to antibodies, with high specificity and affinity to their target molecules. Aptamers can penetrate disease-causing microbial and mammalian cells. Generated aptamers that target surface biomarkers act as cell-targeting agents and intracellular delivery vehicles. Within this context, the "cell-internalizing aptamers" are widely investigated via the process of cell uptake with selective binding during in vivo systematic evolution of ligands by exponential enrichment (SELEX) or by cell-internalization SELEX, which targets cell surface antigens to be receptors. These internalizing aptamers are highly preferable for the localization and functional analyses of multiple targets. In this overview, we discuss the ways by which internalizing aptamers are generated and their successful applications. Furthermore, theranostic approaches featuring cell-internalized aptamers are discussed with the purpose of analyzing and diagnosing disease-causing pathogens.

Matched MeSH terms: Drug Carriers/metabolism*
In Vitro Drug Dissolution/Permeation Testing of Nanocarriers for Skin Application: a Comprehensive Review

Sheshala R, Anuar NK, Abu Samah NH, Wong TW

AAPS PharmSciTech, 2019 Apr 15;20(5):164.
PMID: 30993407 DOI: 10.1208/s12249-019-1362-7

This review highlights in vitro drug dissolution/permeation methods available for topical and transdermal nanocarriers that have been designed to modulate the propensity of drug release, drug penetration into skin, and permeation into systemic circulation. Presently, a few of USFDA-approved in vitro dissolution/permeation methods are available for skin product testing with no specific application to nanocarriers. Researchers are largely utilizing the in-house dissolution/permeation testing methods of nanocarriers. These drug release and permeation methods are pending to be standardized. Their biorelevance with reference to in vivo plasma concentration-time profiles requires further exploration to enable translation of in vitro data for in vivo or clinical performance prediction.

Matched MeSH terms: Drug Carriers*
Folic Acid Conjugated Nanocarriers for Efficient Targetability and Promising Anticancer Efficacy for Treatment of Breast Cancer: A Review of Recent Updates

Choudhury H, Pandey M, Wen LP, Cien LK, Xin H, Yee ANJ, et al.

Curr Pharm Des, 2020;26(42):5365-5379.
PMID: 32693762 DOI: 10.2174/1381612826666200721000958

Breast cancer (BC) is the commonest cause of cancer deaths among Women. It is known to be caused due to mutations in certain receptors, viz. estrogens or progesterones. The most frequently used conventional treatment strategies against BC include chemotherapy, radiation therapy, and partial or entire mastectomy, however, these strategies are often associated with multiple adverse effects, thus reducing patient compliance. Advancement of nanotechnology in the medical application has been made to enhance the therapeutic effectiveness with a significant reduction in the unintended side-effects associated with incorporated anticancer drugs against cancer. The surface engineering technology of the nanocarriers is more pronounced in delivering the therapeutics specifically to target cells. Consequently, folic acid, a small molecular ligand for the folate receptor overexpressed cells, has shown immense response in treating BC cells. Folic acid conjugated nanocarriers have shown remarkable efficiency in targeting overexpressed folate receptors on the surface of BC cells. Binding of these target-specific folate-conjugated nanocarriers substantially improves the internalization of chemotherapeutics in BC cells, without much exposing the other parts of the body. Simultaneously, these folate-- conjugated nanocarriers provide imaging for regular monitoring of targeted drug delivery systems and their responses to an anticancer therapy. Therefore, this review demonstrates the potential of folate-conjugated nanotherapeutics for the treatment and theranostic approaches against BC along with the significant challenges to anticancer therapy, and the prospective insights into the clinical importance and effectiveness of folate conjugate nanocarriers.

Matched MeSH terms: Drug Carriers/therapeutic use
Recent advances in TPGS-based nanoparticles of docetaxel for improved chemotherapy

Choudhury H, Gorain B, Pandey M, Kumbhar SA, Tekade RK, Iyer AK, et al.

Int J Pharm, 2017 Aug 30;529(1-2):506-522.
PMID: 28711640 DOI: 10.1016/j.ijpharm.2017.07.018

Docetaxel (DTX) is one of the important antitumor drugs, being used in several common chemotherapies to control leading cancer types. Severe toxicities of the DTX are prominent due to sudden parenteral exposure of desired loading dose to maintain the therapeutic concentration. Field of nanotechnology is leading to resist sudden systemic exposure of DTX with more specific delivery to the site of cancer. Further nanometric size range of the formulation aid for prolonged circulation, thereby extensive exposure results better efficacy. In this article, we extensively reviewed the therapeutic benefit of incorporating d-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS, or simply TPGS) in the nanoparticle (NP) formulation of DTX for improved delivery, tumor control and tolerability. TPGS is well accepted nonionic-ampiphilic polymer which has been identified in the role of emulsifier, stabilizer, penetration enhancer, solubilizer and in protection in micelle. Simultaneously, P-glycoprotein inhibitory activity of TPGS in the multidrug resistant (MDR) cancer cells along with its apoptotic potential are the added advantage of TPGS to be incorporated in nano-chemotherapeutics. Thus, it could be concluded that TPGS based nanoparticulate application is an advanced approach to improve therapeutic efficacy of chemotherapeutic agents by better internalization and sustained retention of the NPs.

Matched MeSH terms: Drug Carriers/chemistry*
Technical aspects of preparing PEG-PLGA nanoparticles as carrier for chemotherapeutic ‎agents by nanoprecipitation method

Almoustafa HA, Alshawsh MA, Chik Z

Int J Pharm, 2017 Nov 25;533(1):275-284.
PMID: 28943210 DOI: 10.1016/j.ijpharm.2017.09.054

Nanoprecipitation is a simple and increasingly trending method for nanoparticles preparation. The self-assembly feature of poly (ethylene glycol)-poly (lactide-co-glycolic acid) (PEG-PLGA) amphiphilic copolymer into a nanoparticle and its versatile structure makes nanoprecipitation one of the best methods for its preparation. The aim of this study is to review currently available literature for standard preparation of PEG-PLGA nanoparticles using nanoprecipitation technique in order to draw conclusive evidenceto draw conclusive evidence that can guide researchers during formulation development. To achieve this, three databases (Web of Science, Scopus and PubMed) were searched using relevant keywords and the extracted articles were reviewed based on defined inclusion and exclusion criteria. Data extraction and narrative analysis of the obtained literature was performed when appropriate, along with our laboratory observations to support those claims wherever necessary. As a result of this analysis, reports that matched our criteria conformed to the general facts about nanoprecipitation techniques such as simplicity in procedure, low surfactants requirement, narrow size distribution, and low resulting concentrations. However, these reports showed interesting advantages for using PEG-PLGA as they are frequently reported to be freeze-dried and active pharmaceutical ingredients (APIs) with low hydrophobicity were reported to successfully be encapsulated in the particles.

Matched MeSH terms: Drug Carriers/chemistry*
A structurally diverse library of safe-by-design citrem-phospholipid lamellar and non-lamellar liquid crystalline nano-assemblies

Azmi ID, Wibroe PP, Wu LP, Kazem AI, Amenitsch H, Moghimi SM, et al.

J Control Release, 2016 Oct 10;239:1-9.
PMID: 27524284 DOI: 10.1016/j.jconrel.2016.08.011

Non-lamellar liquid crystalline aqueous nanodispersions, known also as ISAsomes (internally self-assembled 'somes' or nanoparticles), are gaining increasing interest in drug solubilisation and bio-imaging, but they often exhibit poor hemocompatibility and induce cytotoxicity. This limits their applications in intravenous drug delivery and targeting. Using a binary mixture of citrem and soy phosphatidylcholine (SPC) at different weight ratios, we describe a library of colloidally stable aqueous and hemocompatible nanodispersions of diverse nanoarchitectures (internal self-assembled nanostructures). This engineered library is structurally stable in human plasma as well as being hemocompatible (non-hemolytic, and poor activator of the complement system). By varying citrem to lipid weight ratio, the nanodispersion susceptibility to macrophage uptake could also be modulated. Finally, the formation of nanodispersions comprising internally V2 (inverse bicontinuous cubic) and H2 (inverse hexagonal) nanoarchitectures was achieved without the use of an organic solvent, a secondary emulsifier, or high-energy input. The tunable binary citrem/SPC nanoplatform holds promise for future development of hemocompatible and immune-safe nanopharmaceuticals.

Matched MeSH terms: Drug Carriers/chemistry*
Polymeric nanoparticles for topical delivery of alpha and beta arbutin: preparation and characterization

Ayumi NS, Sahudin S, Hussain Z, Hussain M, Samah NHA

Drug Deliv Transl Res, 2019 04;9(2):482-496.
PMID: 29569027 DOI: 10.1007/s13346-018-0508-6

To investigate the use of chitosan nanoparticles (CS-TPP-NPs) as carriers for α- and β-arbutin. In this study, CS-TPP-NPs containing α- and β-arbutin were prepared via the ionic cross-linking of CS and TPP and characterized for particle size, zeta potential, and dispersity index. The entrapment efficiency and loading capacity of various β-arbutin concentrations (0.1, 0.2, 0.4, 0.5, and 0.6%) were also investigated. SEM, TEM FTIR, DSC and TGA analyses of the nanoparticles were performed to further characterize the nanoparticles. Finally, stability and release studies were undertaken to ascertain further the suitability of the nanoparticles as a carrier system for α- and β-arbutin. Data obtained clearly indicates the potential for use of CS-TPP-NPs as a carrier for the delivery of α- and β-arbutin. The size obtained for the alpha nanoparticles (α-arbutin CSNPs) ranges from 147 to 274 d.nm, with an increase in size with increasing alpha arbutin concentration. β-arbutin nanoparticles (β-arbutin CSNPs) size range was from 211.1 to 284 dn.m. PdI for all nanoparticles remained between 0.2-0.3 while the zeta potential was between 41.6-52.1 mV. The optimum encapsulation efficiency and loading capacity for 0.4% α-arbutin CSNPs were 71 and 77%, respectively. As for β-arbutin, CSNP optimum encapsulation efficiency and loading capacity for 0.4% concentration were 68 and 74%, respectively. Scanning electron microscopy for α-arbutin CSNPs showed a more spherical shape compared to β-arbutin CSNPs where rod-shaped particles were observed. However, under transmission electron microscopy, the shapes of both α- and β-arbutin CSNP nanoparticles were spherical. The crystal phase identification of the studied samples was carried out using X-ray diffraction (XRD), and the XRD of both α and β-arbutin CSNPs showed to be more crystalline in comparison to their free form. FTIR spectra showed intense characteristic peaks of chitosan appearing at 3438.3 cm-1 (-OH stretching), 2912 cm-1 (-CH stretching), represented 1598.01 cm-1 (-NH2) for both nanoparticles. Stability studies conducted for 90 days revealed that both α- and β-arbutin CSNPs were stable in solution. Finally, release studies of both α- and β-arbutin CSNPs showed a significantly higher percentage release in comparison to α- and β-arbutin in their free form. Chitosan nanoparticles demonstrate considerable promise as a carrier system for α- and β-arbutin, the use of which is anticipated to improve delivery of arbutin through the skin, in order to improve its efficacy as a whitening agent.

Matched MeSH terms: Drug Carriers/chemistry*
Harnessing the dual role of polysaccharides in treating gastrointestinal diseases: As therapeutics and polymers for drug delivery

Corrie L, Gulati M, Awasthi A, Vishwas S, Kaur J, Khursheed R, et al.

Chem Biol Interact, 2022 Dec 01;368:110238.
PMID: 36306865 DOI: 10.1016/j.cbi.2022.110238

Polysaccharides (PS) represent a broad class of polymer-based compounds that have been extensively researched as therapeutics and excipients for drug delivery. As pharmaceutical carriers, PS have mostly found their use as adsorbents, suspending agents, as well as cross-linking agents for various formulations such as liposomes, nanoparticles, nanoemulsions, nano lipid carriers, microspheres etc. This is due to inherent properties of PS such as porosity, steric stability and swellability, insolubility in pH. There have been emerging reports on the use of PS as therapeutic agent due to its anti-inflammatory and anti-oxidative properties for various diseases. In particular, for Crohn's disease, ulcerative colitis and inflammatory bowel disease. However, determining the dosage, treatment duration and effective technology transfer of these therapeutic moieties have not occurred. This is due to the fact that PS are still at a nascent stage of development to a full proof therapy for a particular disease. Recently, a combination of polysaccharide which act as a prebiotic and a probiotic have been used as a combination to treat various intestinal and colorectal (CRC) related diseases. This has proven to be beneficial, has shown good in vivo correlation and is well reported. The present review entails a detailed description on the role of PS used as a therapeutic agent and as a formulation pertaining to gastrointestinal diseases.

Matched MeSH terms: Drug Carriers/chemistry
Diethanolamine-modified pectin based core-shell composites as dual working gastroretentive drug-cargo

Bera H, Kumar S

Int J Biol Macromol, 2018 Mar;108:1053-1062.
PMID: 29122714 DOI: 10.1016/j.ijbiomac.2017.11.019

The current study aimed at developing diethonolamine-modified high-methoxyl pectin (DMP)-alginate (ALG) based core-shell composites for controlled intragastric delivery of metformin HCl (MFM) by combined approach of floating and bioadhesion. DMP with degree of amidation of 48.72% was initially accomplished and characterized by FTIR, DSC and XRD analyses. MFM-loaded core matrices were then fabricated by ionotropic gelation technique employing zinc acetate as cross-linker. The core matrices were further coated by fenugreek gum (FG)-ALG gel membrane via diffusion-controlled interfacial complexation method. Various formulations demonstrated excellent drug encapsulation efficiency (DEE, 51-70%) and sustained drug eluting behavior (Q8h, 72-96%), which were extremely influenced by polymer-blend (ALG:DMP) ratios, low density additives (olive oil/magnesium stearate) and FG-ALG coating inclusion. The drug release profile of the core-shell matrices (F-7) was best fitted in zero-order kinetic model with case-II transport driven mechanism. It also portrayed outstanding gastroretentive characteristics. Moreover, the composites were analyzed for surface morphology, drug-excipients compatibility, thermal behavior and drug crystallinity. Thus, the developed composites are appropriate for controlled stomach-specific delivery of MFM for type 2 diabetes management.

Matched MeSH terms: Drug Carriers/chemistry*
Editorial: Biodegradable Drug Delivery Systems for Cancer Therapy

Wong TW, Sriamornsak P, Dass CR

Curr Drug Deliv, 2018 1 2;14(8):1052.
PMID: 29290178 DOI: 10.2174/156720181408171213150655
Matched MeSH terms: Drug Carriers/chemistry*
Surface Modification of lactose carrier particles using a fluid bed coater to improve fine particle fraction for dry powder inhalers

Gong QQ, Tay JYS, Veronica N, Xu J, Heng PWS, Zhang YP, et al.

Pharm Dev Technol, 2023 Feb;28(2):164-175.
PMID: 36683577 DOI: 10.1080/10837450.2023.2171434

Surface roughness of carrier particles can impact dry powder inhaler (DPI) performance. There are opposing views on the effect of roughness on DPI performance. Hence, a systematic approach is needed to modify carrier surfaces and evaluate the impact on drug delivery. Carrier particle surfaces were modified by fluid bed coating with saturated lactose containing micronized lactose of different sizes (2, 5 and 8 μm) and coated to different levels (20, 40, 60 and 80%). Their drug delivery performance was assessed by the fine particle fraction (FPF). Roughness parameters, mean arithmetic roughness (Ra) and arithmetic mean height (Sa), of the carrier particles, were also evaluated using optical profilometry and scanning laser microscopy. Generally, particles of higher Ra had higher FPF. Higher Sa resulted in higher FPF only for particles with 60 and 80% coat levels. Reduced contact surface area between the drug particle and rougher carrier particle resulted in easier drug detachment during aerosolization. The 5 µm micronized lactose produced optimal carrier particles with respect to FPF and surface roughness. The study highlighted that with the ideal particles for surface roughening and coating level, surface roughening could be efficiently achieved by fluid bed coating for superior DPI performance.

Matched MeSH terms: Drug Carriers*
Recent advancement on albumin nanoparticles in treating lung carcinoma

Sristi, Fatima M, Sheikh A, Almalki WH, Talegaonkar S, Dubey SK, et al.

J Drug Target, 2023 Jun;31(5):486-499.
PMID: 37125741 DOI: 10.1080/1061186X.2023.2205609

With the advancement of nanotechnology, many different forms of nanoparticles (NPs) are created, which specifically enhance anticancer drug delivery to tumour cells. Albumin bio-macromolecule is a flexible protein carrier for the delivery of drugs that is biodegradable, biocompatible, and non-toxic. As a result, it presents itself as an ideal material for developing nanoparticles for anticancer drug delivery. Toxicological investigations demonstrated that this novel drug delivery technique is safe for use in the human population. Furthermore, drug compatibility with the albumin nanoparticle is remarkable. The robust structure of the nanoparticle, high drug encapsulation, and customisable drug release make it a promising carrier option for the treatment of lung cancer. In this review, we summarise human serum albumin and bovine serum albumin in the targeted delivery of anticancer drugs to lung cancer cells.

Matched MeSH terms: Drug Carriers/chemistry
Transethosome: An ultra-deformable ethanolic vesicle for enhanced transdermal drug delivery

Raj A, Dua K, Nair RS, Sarath Chandran C, Alex AT

Chem Phys Lipids, 2023 Sep;255:105315.
PMID: 37356610 DOI: 10.1016/j.chemphyslip.2023.105315

Drug delivery through the skin improves solubility, bioavailability, and unwanted systemic side effects of the drug. The selection of a suitable carrier is a challenging process. The conventional lipid vesicles have some limitations. They deliver the drug in the stratum corneum and have poor colloidal stability. Here comes the need for ultra-deformable lipid vesicles to provide the drug beyond the stratum corneum. Transethosomes are novel ultra-deformable vesicles that can deliver drugs into deeper tissues. The composition of transethosomes includes phospholipid, ethanol and surfactants. Each ingredient has a pivotal role in the properties of the carrier. This review covers the design, preparation method, characterisation, and characteristics of the novel vesicle. Also, we cover the impact of surfactants on vesicular properties and the skin permeation behaviour of novel vesicles.

Matched MeSH terms: Drug Carriers/metabolism

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